The present invention relates to a compound having a structure in which methotrexate and a peptide are connected via a covalent bond, and an anticancer or anti-inflammatory pharmaceutical composition comprising same. The compound having a structure in which methotrexate and a peptide are connected via a covalent bond of the present invention has excellent biological activity such as anticancer or anti-inflammatory action and has markedly reduced toxicity with respect to cells, and thus, may be usefully used in various fields such as medicine and medical supplies.